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Also known as LY4064809 Test Formulation, STX-478, Tersolisib, [14C]-STX-478
LY4064809 · 3 trials · 5 indications
As determined by the investigator based on Response Evaluation Criteria in Solid Tumors (RECIST) v 1.1
Investigator-assessed
| Arm | Type | Description |
|---|---|---|
| LY4064809 + CDK4/6 Inhibitor + Endocrine Therapy (ET) (Part 1) | EXPERIMENTAL | LY4064809 given orally in one of two doses in combination with investigator's choice of CDK4/6 inhibitor given orally and ET given orally or intramuscularly |
| LY4064809 + CDK4/6 Inhibitor + Endocrine Therapy (ET) (Part 2) | EXPERIMENTAL | LY4064809 given orally in combination with CDK4/6 inhibitor given orally and ET given orally or intramuscularly |
| Placebo + CDK4/6 Inhibitor + Endocrine Therapy (ET) (Part 2) | PLACEBO_COMPARATOR | Placebo given orally in combination with CDK4/6 inhibitor given orally and ET given orally or intramuscularly |
| Group 1 Treatment A Fasted | EXPERIMENTAL | Tersolisib administered orally. |
| Group 1 Treatment B High-Fat Meal | EXPERIMENTAL | Tersolisib administered orally. |
| Group 2 Treatment A Fasted | EXPERIMENTAL | Tersolisib administered orally. |
| Group 2 Treatment C Low-Fat Meal | EXPERIMENTAL | Tersolisib administered orally. |
| Dose Escalation (Advanced Solid Tumors) | EXPERIMENTAL | * Cohort A0: Advanced Solid tumors expressing PI3Kα mutations * Cohort A1: HR+ breast cancer expressing PI3Kα mutations |
| Dose Expansion | EXPERIMENTAL | * Cohort A2: Gynecologic cancers * Cohort A3: Head and Neck Squamous Cell Carcinoma * Cohorts A4/A5: Other solid tumors not included in Cohorts A1, A2, A3 expressing PI3Kα mutations * Cohort A6: Endometrial cancer * Cohort A7: Non-gastrointestinal solid tumors |
| Dose Selection/Expansion: Combination STX-478 + fulvestrant | EXPERIMENTAL | Cohort B: HR+/HER2- or HR+/HER2low breast cancer expressing PI3Kα mutations |
| Dose Selection/Expansion Combination | EXPERIMENTAL | STX-478 + Endocrine therapy + CDK4/6 inhibitor Cohort C/D/E: HR+/HER2- or HR+/HER2low breast cancer expressing PI3Ka mutations |
| Experimental: Drug to Drug Interaction (DDI) Metformin STX-478 +/- ET ([AIs or fulvestrant] | EXPERIMENTAL | CDK4/6 inhibitor therapy in Cohort A8: all solid tumors Cohort B2 and Cohort F: HR+/HER2- or HR+/HER2 low breast cancer expressing PI3Kα mutations |
| Name | Type | Description |
|---|---|---|
| LY4064809 | DRUG | Administered orally |
| Placebo | DRUG | Administered orally |
| Ribociclib | DRUG | Administered orally |
| Palbociclib | DRUG | Administered orally |
| Abemaciclib | DRUG | Administered orally |
| Anastrozole | DRUG | Administered orally |
| Letrozole | DRUG | Administered orally |
| Exemestane | DRUG | Administered orally |
| Fulvestrant | DRUG | Administered intramuscular |
| Tersolisib | DRUG | Tersolisib administered orally |
| High-fat Meal | OTHER | High-fat Meal |
| Low-fat Meal | OTHER | Low-fat Meal |
| STX-478 | DRUG | STX-478 is a mutant-selective PI3Kα inhibitor |
| Tamoxifen | DRUG | Tamoxifen |
| Imlunestrant | DRUG | Imlunestrant |
| Metformin | DRUG | Metformin |
Inclusion Criteria: * Are willing to follow contraception requirements. Contraceptive use by participants should be consistent with local regulations regarding the methods of contraception for those participating in clinical trials. * If assigned female at birth, pre-/peri- and postmenopausal statu...
LY4064809 is an investigational small molecule drug being developed by Eli Lilly and Company for breast neoplasms, including metastatic disease. It is a PIK3CA-targeted therapy given to patients whose tumors carry a PIK3CA genetic change. It is currently in Phase 3 clinical development and has not been approved by the FDA.
LY4064809 is being studied for advanced breast cancer, including neoplasm metastasis, in participants whose tumors have a PIK3CA genetic change. The Phase 3 trial evaluates the drug in combination with other anti-cancer treatments. It is investigational and is not approved for any use.
LY4064809 targets PIK3CA, a gene that encodes a component of the PI3K signaling pathway. The drug is designed for biomarker-selected patients, meaning treatment is directed at tumors that carry a PIK3CA genetic change. This targeted approach distinguishes it from non-selective breast cancer therapies.
LY4064809 is developed by Eli Lilly and Company, which trades on the New York Stock Exchange under the ticker LLY. Lilly is running the clinical development program for the drug in advanced breast cancer. The compound is also referred to in study documentation as LY4064809/STX-478.
LY4064809 is in Phase 3 clinical development. It is investigational and has not been approved by the FDA. The Phase 3 study is randomized, double-blind, and placebo-controlled, and it is currently recruiting participants. Enrollment is planned for 800 participants.
LY4064809 is being studied in one active Phase 3 trial, NCT07174336, titled A Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA). The trial is recruiting 800 participants across the United States, Europe, Asia, Latin America, Australia, and Turkey.
Yes. LY4064809 is also known as LY4064809 Test Formulation, and study documentation additionally refers to it as LY4064809/STX-478 and tersolisib. These names refer to the same investigational PIK3CA-targeted small molecule developed by Eli Lilly and Company for advanced breast cancer.